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Pronunciation |
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(a
mee noe ka PROE ik AS
id) |
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U.S. Brand
Names |
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Amicar® |
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Generic
Available |
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Yes: Injection |
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Pharmacological Index |
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Hemostatic Agent |
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Use |
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Treatment of excessive bleeding from fibrinolysis |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Disseminated intravascular coagulation, hematuria of upper urinary tract, use
of Factor IX concentrate or Anti-inhibitor coagulant
concentrate |
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Warnings/Precautions |
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Rapid I.V. administration of the undiluted drug is not recommended;
aminocaproic acid may accumulate in patients with decreased renal function; do
not use in hematuria of upper urinary tract origin unless possible benefits
outweigh risks; use with caution in patients with cardiac, renal or hepatic
disease; do not administer without a definite diagnosis of laboratory findings
indicative of hyperfibrinolysis; use in breast-feeding women is not
recommended |
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Adverse
Reactions |
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1% to 10%:
Cardiovascular: Hypotension, bradycardia, arrhythmia
Central nervous system: Dizziness, headache, malaise, fatigue
Dermatologic: Rash
Gastrointestinal: GI irritation, nausea, cramps, diarrhea
Hematologic: Decreased platelet function, elevated serum enzymes
Neuromuscular & skeletal: Myopathy, weakness
Otic: Tinnitus
Respiratory: Nasal congestion
<1%: Convulsions, ejaculation problems, rhabdomyolysis, renal failure
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Overdosage/Toxicology |
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Symptoms of overdose include nausea, diarrhea, delirium, hepatic necrosis,
thromboembolism |
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Drug
Interactions |
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Increased toxic effect with oral contraceptives,
estrogens |
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Mechanism of
Action |
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Competitively inhibits activation of plasminogen to plasmin, also, a lesser
antiplasmin effect |
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Pharmacodynamics/Kinetics |
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Oral: Peak effect: Within 2 hours; Therapeutic effect: Within 1-72 hours
after dose
Distribution: Widely distributes through intravascular and extravascular
compartments
Metabolism: Minimal hepatic
Half-life: 1-2 hours
Elimination: 68% to 86% excreted as unchanged drug in urine within 12 hours
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Usual Dosage |
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In the management of acute bleeding syndromes, oral dosage regimens are the
same as the I.V. dosage regimens in adults and children
Acute bleeding syndrome:
Children: Oral, I.V.: 100 mg/kg or 3 g/m2 during the first hour,
followed by continuous infusion at the rate of 33.3 mg/kg/hour or 1
g/m2/hour; total dosage should not exceed 18 g/m2/24 hours
Traumatic hyphema: Oral: 100 mg/kg/dose every 6-8 hours
Adults:
Oral: For elevated fibrinolytic activity, administer 5 g during first hour,
followed by 1-1.25 g/hour for approximately 8 hours or until bleeding stops
I.V.: 4-5 g in 250 mL of diluent during first hour followed by continuous
infusion at the rate of 1-1.25 g/hour in 50 mL of diluent, continue for 8 hours
or until bleeding stops
Maximum daily dose: Oral, I.V.: 30 g
Dosing adjustment in renal impairment: Oliguria or ESRD: Reduce dose
by 15% to 25% |
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Monitoring
Parameters |
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Fibrinogen, fibrin split products, creatine phosphokinase (with long-term
therapy) |
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Reference Range |
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Therapeutic concentration: >130 mg/mL
(concentration
necessary for inhibition of fibrinolysis) |
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Test
Interactions |
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potassium, creatine
phosphokinase [CPK]
(S) |
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Mental Health: Effects
on Mental Status |
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May cause drowsiness |
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Mental Health:
Effects on Psychiatric
Treatment |
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May cause hypotension which may be exacerbated by psychotropics; rarely may
cause seizures; use caution with clozapine and bupropion |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take oral medication exactly as directed. This medication may cause dizziness
and fatigue (use caution when driving or engaging in tasks that require
alertness until response to drug is known); hypotension (use caution when rising
from a lying or sitting position or climbing stairs); menstrual irregularities,
increased body hair, or sexual dysfunction (should reverse when treatment is
completed); or nausea or vomiting (small frequent meals, frequent mouth care,
sucking lozenges, or chewing gum may help). Report immediately chest pain;
dyspnea; swelling; nosebleed; warmth, swelling, pain, or redness in calves; skin
rash; muscle pain or weakness; ringing in ears; or acute abdominal cramping.
Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend
to be pregnant. Consult prescriber if breast-feeding. |
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Nursing
Implications |
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Administration by infusion using appropriate I.V. solution (dextrose 5% or
sodium chloride 0.9%); rapid I.V. injection (IVP) should be avoided since
hypotension, bradycardia, and arrhythmia may result. Aminocaproic acid may
accumulate in patients with decreased renal function. |
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Dosage Forms |
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Injection: 250 mg/mL (20 mL, 96 mL, 100 mL)
Syrup: 1.25 g/5 mL (480 mL)
Tablet: 500 mg |
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References |
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Korzenik JR, Topazian MD, and White R,
"Treatment of Bleeding in Hereditary Hemorrhagic Telangiectasia With Aminocaproic Acid,"
N Engl J Med, 1994, 331(18):1236.
McGetrick JJ, Jampol LM, Goldberg MP, et al,
"Aminocaproic Acid Decreases Secondary Hemorrhage After Traumatic Hyphema,"
Arch Ophthalmol, 1983, 101(7):1031-3.
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